Seralutinib

Seralutinib is an inhibitor of PDGFR, c-Kit, and colony stimulating factor 1 receptor (CSF1R). It inhibits PDGF-BB-induced phosphorylation of ERK in PDGFRalpha-dependent H1703 human lung epithelial cells, human pulmonary arterial smooth muscle cells (HPASMCs), which express PDGFRalpha and PDGFRbeta, and human lung fibroblasts (HLFs), which express higher levels of PDGFRbeta than PDGFRalpha (IC50s = 74, 49, and 62 nM, respectively). Seralutinib also inhibits stem cell factor-induced c-Kit autophosphorylation in human pulmonary endothelial cells (HPAECs) and M-CSF-induced CSF1R phosphorylation in human primary differentiated macrophages (IC50s = 7.8 and 14.4 nM, respectively). It inhibits the proliferation of H1703 cells and PDGF-BB-induced HPASMCs and HLFs (IC50s = 32, 33, and 29 nM, respectively). Seralutinib (2.5 mg/kg) prevents increases in pulmonary artery systolic pressure in a rat model of pulmonary arterial hypertension induced by monocrotaline (Cay-16666) pneumonectomy when administered via passive inhalation.Formal Name: N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-3-pyridinecarboxamide. CAS Number: 1619931-27-9. Synonyms: GB002, PK 10571. Molecular Formula: C27H27N5O3. Formula Weight: 469.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 25 mg/ml, Ethanol: 10 mg/ml. lambdamax: 273 nm. SMILES: COC1=C(OC)C=CC(C2=NC(N[C@H](C3=CC(NC(C4=CN=CC(C)=C4)=O)=CC=C3)C)=CN=C2)=C1. InChi Code: InChI=1S/C27H27N5O3/c1-17-10-21(14-28-13-17)27(33)31-22-7-5-6-19(11-22)18(2)30-26-16-29-15-23(32-26)20-8-9-24(34-3)25(12-20)35-4/h5-16,18H,1-4H3,(H,30,32)(H,31,33)/t18-/m0/s1. InChi Key: JHJNPOSPVGRIAN-SFHVURJKSA-N.